Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Derazantinib (ARQ-087) 是一种有效的,ATP 竞争型的,具有口服活性的酪氨酸激酶抑制剂,能够抑制软骨细胞FGFR1 (IC50:4.5 nM)、FGFR2 (IC50:1.8 nM)、FGFR3 (IC50:4.35nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 656 | 现货 | ||
2 mg | ¥ 955 | 现货 | ||
5 mg | ¥ 1,570 | 现货 | ||
10 mg | ¥ 2,890 | 现货 | ||
25 mg | ¥ 4,850 | 现货 | ||
50 mg | ¥ 6,890 | 现货 | ||
100 mg | ¥ 9,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,630 | 现货 |
产品描述 | Derazantinib (ARQ-087) (ARQ-087) is an ATP competitive tyrosine kinase inhibitor. It exhibits potent activity against FGFR1/FGFR2/FGFR3 chondrocytes (IC50s: 4.5 nM/1.8 nM/4.5 nM). |
靶点活性 | FGFR2:1.8 nM, FGFR1:4.5 nM, FGFR3:4.5 nM |
体外活性 | In cells, inhibition of FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK) is evident by the response to Derazantinib treatment. Derazantinib has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations. Cell cycle studies in cell lines with high levels of FGFR2 protein show a positive relationship between Derazantinib induced G1 cell cycle arrest and subsequent induction of apoptosis [1]. Derazantinib rescues the FGF2-mediated growth arrest with EC50 at about 100 nM, with no significant toxicity detected for up to 500 nM. The concentration range at which Derazantinib significantly suppresses the FGF2 effect is between 70-500 nM. Derazantinib inhibits FGF-mediated loss of extracellular matrix and induction of chondrocyte premature senescence. Derazantinib rescues FGF-mediated inhibition of chondrocyte differentiation in tibia cultures. Derazantinib inhibits FGFR1-4 but no other receptor tyrosine kinases in the cell-free kinase assay. Derazantinib inhibits FGFR1 and FGFR2 mutants associated with craniosynostoses [2]. |
体内活性 | Derazantinib is effective at inhibiting tumor growth in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplification and fusions [1]. Most of the embryos exhibit abnormal external phenotype (81.3%) in Derazantinib-injected wings, possibly due to inhibition of proliferation of limb bud mesenchyme [2]. |
激酶实验 | Derazantinib is titrated in DMSO utilizing a 3-fold dilution scheme and then diluted 10-fold further in deionized water for a final DMSO concentration of 10%. A volume (2.5 μL) of these dilutions or vehicle is added to each well of a reaction plate. FGFR1 or FGFR2 is added to assay buffer to each well in a volume of 17.5 μL for a final concentration of 0.50 or 0.25 nM, respectively. After a 30-minute pre-incubation period, ATP and substrate are added in assay buffer (5 μL) for final concentrations of 0-1,000 μM ATP and 80 nM biotinylated-PYK2, for a final reaction volume of 25 μL. The plates are incubated for 60 minutes at room temperature and then stopped in the dark by the addition of 10 μL stop/detection mixture prepared in assay buffer containing EDTA [1]. |
细胞实验 | Cells are seeded at 3000-5000 cells per well with 130 μL media in 96-well tissue culture-treated plates. The cells are incubated overnight and subsequently treated with 3-fold serial dilutions of Derazantinib starting at 100 μM. The cells are returned to a 37°C humidified incubator for 72 hours. Cell proliferation is measured using the MTS assay [1]. |
动物实验 | Female NCr nu/nu mice (SNU-16) or CB17 SCID mice (NCI-H716) with well established (400 mg) subcutaneous tumors are given a single oral dose of Derazantinib or vehicle control. Plasma and tumor samples are collected 4 hours post single dose. Derazantinib is administered orally. The dosing volume for all groups is 10 mL/kg or 0.1 mL/10 g body weight [1]. |
别名 | ARQ-087 |
分子量 | 468.57 |
分子式 | C29H29FN4O |
CAS No. | 1234356-69-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 98 mg/mL (209.15 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1342 mL | 10.6708 mL | 21.3415 mL | 53.3538 mL |
5 mM | 0.4268 mL | 2.1342 mL | 4.2683 mL | 10.6708 mL | |
10 mM | 0.2134 mL | 1.0671 mL | 2.1342 mL | 5.3354 mL | |
20 mM | 0.1067 mL | 0.5335 mL | 1.0671 mL | 2.6677 mL | |
50 mM | 0.0427 mL | 0.2134 mL | 0.4268 mL | 1.0671 mL | |
100 mM | 0.0213 mL | 0.1067 mL | 0.2134 mL | 0.5335 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Derazantinib 1234356-69-4 Angiogenesis Tyrosine Kinase/Adaptors FGFR ARQ-087 ARQ087 Fibroblast growth factor receptor inhibit ARQ 087 Inhibitor inhibitor